pparγ lbd

Leriglitazone is a brain barrier-permeable, orally active PPARγ agonist (EC50=9 μM) and mitochondrial function modulator with neuroprotective, anti-inflammatory, and antioxidant properties for neurodegenerative disease research.

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

PPARγmodulator-2 (Compound (R)-2n) is a reversible modulator of PPARγ, inhibiting the PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. It helps lower blood glucose levels, improves glucose tolerance and insulin sensitivity, and demonstrates antidiabetic activity in db/db mouse models.

Leriglitazone (Hydroxypioglitazone) hydrochloride, a pioglitazone metabolite, acts as a PPARγ agonist, effectively stabilizing the PPARγ activation function-2 (AF-2) co-activator binding surface to enhance co-activator binding, which results in a modest improvement in transcriptional efficacy. It binds to the PPARγ C-terminal ligand-binding domain (LBD) with a dissociation constant (K i) of 1.2 μM and demonstrates transcriptional efficacy with an effective concentration (EC 50) of 680 nM [1].